Wpis z mikrobloga

Why is it consumed via the nose and not some other way?


Bioavailability. Cocaine has an extraordinarily low oral bioavailability, meaning not much actually gets absorbed into the bloodstream when you swallow it.

It is most commonly taken intranasally (via insufflation/"snorting"), bucally (by rubbing it under the gums), rectally ("boofing"), via inhalation, or intravenously.

Most people don't like sticking drugs up their ass, so they don't boof. It's an acquired taste, and numbs the gums, so people don't usually use it bucally unless they're using raw coca leaves.

Intravenous bioavailability for any drug is 100%, since bioavailability is a measure of the amount of the drug that makes it into your bloodstream, but most people don't like injecting themselves with needles (and for good reason).

This leaves smoking and snorting as the two main ways people use cocaine. However, the hydrochloride salt of cocaine doesn't vapourize very well, so smoking only works well with freebase cocaine (colloquially known as "crack").

So, TL;DR:

The intranasal bioavailability of cocaine is ~80%, and most other routes of administration are either physically unsafe or simply unpleasant.

Moving on to the mechanism of action:

Cocaine has two primary mechanisms of action.

It acts as an inhibitor of voltage-gated sodium channels, which can lead to heart attacks by dysregulating cardiac activity. This is why cocaine is responsible for more lethal overdoses than any other stimulant known to man.

Sodium channels are also involved in perception of sensation, which is why it produces a topical & systemic numbing effect. The primary use of the coca plant throughout history was as an anaesthetic, precisely for this reason.

However, the majority of the psychoactive effects come from its activity as an NDRI (norepinephrine-dopamine reuptake inhibitor).

Neurotransmitters are stored in the cytosol, and when they're "released", it means they're released into the synaptic cleft, where their receptors are located.

Promptly after release, they are returned by their respective transporters into the cytosol of the neuron in a process known as "reuptake".

A reuptake inhibitor blocks this transporter, preventing the reuptake process, making that neurotransmitter active for longer.

So, TL;DR:

Cocaine blocks sodium channels & also increases the concentration of dopamine and norepinephrine in the synaptic cleft

#kokaina
  • Odpowiedz